Halofuginone

製品コードS8144 バッチS814401

印刷

化学情報

Chemical Structure Synonyms RU-19110 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H17BrClN3O3
分子量 414.68 CAS No. 55837-20-2
Solubility (25°C)* 体外 DMSO 8 mg/mL (19.29 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5% DMSO 95% Corn oil
0.4mg/ml Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
0.4mg/ml Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Halofuginone (RU-19110) is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal.
in vitro In mammals, halofuginone at 10 ng/ml down-regulates Smad3, blocking TGF-β signaling and preventing both the differentiation of fibroblasts to myofibroblasts and the transitioning of epithelial cells to mesenchymal cells[2].
in vivo Halofuginone clearly extends the survival times of the parasite-infected mice. Oral treatment with halofuginone at doses of 0.2 and 1 mg/kg has an apparent curative effect for the infected mice. The subcutaneous administration of 0.2 mg of halofuginone per kg likewise extends the survival times of the infected mice, but none of the mice is cured. The mice in the 5-mg/kg dose groups die before the completion of treatment with the drug either orally or subcutaneously. Subcutaneous treatment with halofuginone appears to be more toxic to mice than oral treatment[3].

プロトコル(参考用のみ)

キナーゼアッセイ Assay of ProRS activity
The prolyl tRNA synthetase domain of human EPRS (ProRS) is expressed in E.coli with a 6-his tag and purified. Enzymatic activity is assayed using incorporation of 3H Pro into the tRNA fraction essentially, except that the charged tRNA fraction is isolated by rapid batchwise binding to Mono Q sepharose and quantitated by liquid scintillation counting. For all kinetic assays, the concentration of active enzyme in the reaction is 40 nM. Similar inhibition by HF is seen using the human ProRS domain purified from bacteria and full length EPRS purified from rat liver.
細胞アッセイ 細胞株 primary murine CD4+ CD25− T cells/MEFs
濃度 5-20nM
反応時間 4 or 24hrs
実験の流れ

Primary murine CD4+ CD25− T cells are activated through the TCR in Th17 polarizing conditions in the presence of either 10nM MAZ1310 or HF and amino acid supplements. Th17 differentiation is assayed in the absence or presence of HF or borrelidin, with or without 1 mM threonine or proline supplementation. MEFs are treated with or without HF (50 nM) and/or Proline (2 mM) for 4 hours (CHOP, S100A4) or 24 hours (ColIA1, Col1A2). 
動物実験 動物モデル 4- to 5-week-old ICR mice
投薬量 0.2 and 1 mg/kg
投与方法 Oral treatment/subcutaneous administration

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

EPRS1 correlates with malignant progression in hepatocellular carcinoma [ Infect Agent Cancer, 2023, 18(1):27] PubMed: 37138286
Transforming growth factor-β receptor type 2 is required for heparin-binding protein-induced acute lung injury and vascular leakage for transforming growth factor-β/Smad/Rho signaling pathway activation [ FASEB J, 2022, 36(11):e22580] PubMed: 36189652
Integrated Stress Response Regulation of Corneal Epithelial Cell Motility and Cytokine Production [ Invest Ophthalmol Vis Sci, 2022, 63(8):1] PubMed: 35802384
Cancer-associated fibroblasts-derived HAPLN1 promotes tumour invasion through extracellular matrix remodeling in gastric cancer [ Gastric Cancer, 2021, 10.1007/s10120-021-01259-5] PubMed: 34724589
SARS-CoV-2 spike protein 13-mer subdomain corresponds to the drug-binding domain of glutamyl-propyl-tRNA synthetase 1 and is targetable by halofuginone [ Research Square, 2021, 10.21203/rs.3.rs-738132/v1] PubMed: None
Red-COLA1: a human fibroblast reporter cell line for type I collagen transcription [ Sci Rep, 2020, 10(1):19723] PubMed: 33184327
Halofuginone inhibits tumorigenic progression of 5-FU-resistant human colorectal cancer HCT-15/FU cells by targeting miR-132-3p in vitro [ Oncol Lett, 2020, 20(6):385] PubMed: 33154782
A high throughput screen for TMPRSS2 expression identifies FDA-approved and clinically advanced compounds that can limit SARS-CoV-2 entry [ Res Sq, 2020, rs.3.rs-48659] PubMed: 32818215

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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